Assay Detail
Binding
CHEMBL654576
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit [3H]nitrendipine binding to the calcium channel receptor(CCR) in rat cerebral cortex homogenate.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Voltage-gated L-type calcium channel (CHEMBL2095177) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.52 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL33165 | — | — | 1 | 9.89 |
| CHEMBL277363 | — | — | 1 | 9.38 |
| CHEMBL328609 | — | — | 1 | 8.48 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 8.43 |
| CHEMBL284623 | — | — | 1 | 8.31 |
| CHEMBL33083 | — | — | 1 | 8.22 |
| CHEMBL33609 | — | — | 1 | 7.80 |
| CHEMBL318007 | — | — | 1 | 7.66 |
| CHEMBL100709 | — | — | 1 | 7.54 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 7.34 |
| CHEMBL32657 | — | — | 1 | 6.88 |
| CHEMBL319316 | — | — | 1 | 6.87 |
| CHEMBL33042 | — | — | 1 | 6.82 |
| CHEMBL98834 | — | — | 1 | 6.52 |
| CHEMBL33096 | — | — | 1 | 6.38 |
| CHEMBL430463 | — | — | 1 | 6.02 |
| CHEMBL102052 | — | — | 1 | 5.28 |
| CHEMBL33488 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL33165 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL277363 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL328609 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL284623 | — | IC50 | = | 4.88 | nM | 8.31 |
| CHEMBL33083 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL33609 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL318007 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL100709 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL32657 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL319316 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL33042 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL98834 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL33096 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL430463 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL102052 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL33488 | — | IC50 | > | 2000.0 | nM | - |